Seizures
- Focal -only a portion of brain or hemisphere
- Simple - single limb or muscle group,no loss of consciousness
- Complex - chewing movements, diarrhea, urination ,with loss of consciousness
- Generalized - immediate loss of consciousness
- Absence - rapid eye blinking for 3-5 seconds
- Myoclonic - short episode of muscle contraction
- Tonic - increased tone in extensor muscles for 60 seconds
- Clonic - muscle contraction with more altered consciousness
- Tonic clonic - continuous contraction and rapid movement
- Atonic - sudden loss of muscle tone
- Simple - single limb or muscle group,no loss of consciousness
- Complex - chewing movements, diarrhea, urination ,with loss of consciousness
- Absence - rapid eye blinking for 3-5 seconds
- Myoclonic - short episode of muscle contraction
- Tonic - increased tone in extensor muscles for 60 seconds
- Clonic - muscle contraction with more altered consciousness
- Tonic clonic - continuous contraction and rapid movement
- Atonic - sudden loss of muscle tone
Epilepsy
Predisposition to recurrent unprovoked seizures
Mechanisms
- Abnormal neuronal circuits
- Channellopathis
- Increased excitation
- increased Na influx
- increased Ca influx
- decreased K efflux
- Decreased inhibition
- reduced GABA activity
Treatment Methods- Ion channel block
- Na
- Ca
- Reduce Glutamate activity
- Increase GABA activity
- increase post synaptic action of GABA
- decrease GABA transaminases
- decrease GABA re uptake in to glial cells
1. PHENITOIN
- Use dependent Na channel blocker
- only inactivated Na channels will be blocked(so only repetitively discharging & high frequent channels)
- slowly absorbed (85%) metabolized by the liver
- half life 12-36 h
- CYP450 inducer
- metabolism is increased by - Phenobarbitone, Valproate, Isoniazid
- ADE
- Cosmetic - gum hyperplasia , acne , hirsutism , focal coarsening
- cognitive impairment
- osteomalacia
- megaloblastic anaemia
- teratogenic
- Toxicity - drowsiness , diplopia , dysarthria
- Uses
- Status epilepticus
- Trigeminal neuralgia
- Myotonic dystrophy
2.CARBAMEZAPINE
- Na channel blocker
- CYP450 inducer
- no loading doses as it ca cause toxicity
- ADE
- rash
- drowsiness, imbalance, diplopia, ataxia
- rarely - agranulocytosis, SIADH, hyponatreamia
- folic acid defeciency & osteomalacia
- Uses
- partial seizures
- neuropathic pain
- maniac depressive illness
- Ox carbamezapine
- similar pro drug with less enzyme induction
3.LAMOTRIGINE
- Action
- Na channel block
- Ca channel block
- reduce Glutamate release
- metabolized by liver.
- increased by - phenytoin, carbomezapine, phenobarbitone
- reduced by - valproate
- Uses
- partial/generalized seizures
- absence seizures
4.SODIUM VALPROATE
- Action
- Na channel block
- T type Ca channel blok
- GABA potentiation
- inhibit GABA transaminases
- CYP450 Inducer
- ADE
- dyspepsia
- tremor
- weight gain
- impaired glucose tolerance
- hepatotoxic
- teratogenic - neural tube defects
- hair loss
- Uses
- Tonic clonic
- Bipolar depressive disorder
- Absence seizures
5.PHENOBARBITONE
- Action
- potentiate GABA receptor activation
- CYP450 inducer
- half life 72 - 144 h
- ADE
- sedation with therapeutic levels
- changes in cognition, mood & behaviour
- megaloblastic changes
- osteomalacia
- hypersensitive reaction
- addiction
- depress brain stem functions
- coma, respiratory failure, cardiac arrest
6.CLONAZAPAM
- Action
- enhance GABA receptor activation
- T type Ca channel inhibition
- ADE
- sedation
- tolerance with prolong use
7.VIGABATRIN
- Action
- Irreversible inhibition of GABA transaminases
- ADE
- tunnel vision - 6 month visual field monitoring
8.GABAPENTIN
- Action
- inhibit Glutamate release by blocking high voltage Ca channels
- No effect on metabolizing enzymes
- eliminated unchanged in urine
- half life is 6h so given tds
- ADE
- sedation
- fatigue
- weightgain
- Uses
- adjunctive therapy for partial seizures
9.TOPIRAMATE
- Action
- Na ,Ca channel block
- GABA potentiation
- Glutamate receptor block
- Carbonic anhydrase inhibitor
- ADE
- sedation
- fatigue
- renal calculi
- weight loss
- increased intra occular pressure
10.LEVATIRACETAM
- Action
- inhibit Glutamate release
- renal elimination- unchanged
- Uses
- migraine prevention
- partial seizures
11.ETHOSUXIMIDE
Carbamezapine is relatively safe in pregnancy with vit K & folic acid supplementation.
- Abnormal neuronal circuits
- Channellopathis
- Increased excitation
- increased Na influx
- increased Ca influx
- decreased K efflux
- Decreased inhibition
- reduced GABA activity
Treatment Methods
- Ion channel block
- Na
- Ca
- Reduce Glutamate activity
- Increase GABA activity
- increase post synaptic action of GABA
- decrease GABA transaminases
- decrease GABA re uptake in to glial cells
1. PHENITOIN
- Use dependent Na channel blocker
- only inactivated Na channels will be blocked(so only repetitively discharging & high frequent channels)
- slowly absorbed (85%) metabolized by the liver
- half life 12-36 h
- CYP450 inducer
- metabolism is increased by - Phenobarbitone, Valproate, Isoniazid
- ADE
- Cosmetic - gum hyperplasia , acne , hirsutism , focal coarsening
- cognitive impairment
- osteomalacia
- megaloblastic anaemia
- teratogenic
- Toxicity - drowsiness , diplopia , dysarthria
- Uses
- Status epilepticus
- Trigeminal neuralgia
- Myotonic dystrophy
2.CARBAMEZAPINE
- Na channel blocker
- CYP450 inducer
- no loading doses as it ca cause toxicity
- ADE
- rash
- drowsiness, imbalance, diplopia, ataxia
- rarely - agranulocytosis, SIADH, hyponatreamia
- folic acid defeciency & osteomalacia
- Uses
- partial seizures
- neuropathic pain
- maniac depressive illness
- Ox carbamezapine
- similar pro drug with less enzyme induction
3.LAMOTRIGINE
- Action
- Na channel block
- Ca channel block
- reduce Glutamate release
- metabolized by liver.
- increased by - phenytoin, carbomezapine, phenobarbitone
- reduced by - valproate
- Uses
- partial/generalized seizures
- absence seizures
4.SODIUM VALPROATE
- Action
- Na channel block
- T type Ca channel blok
- GABA potentiation
- inhibit GABA transaminases
- CYP450 Inducer
- ADE
- dyspepsia
- tremor
- weight gain
- impaired glucose tolerance
- hepatotoxic
- teratogenic - neural tube defects
- hair loss
- Uses
- Tonic clonic
- Bipolar depressive disorder
- Absence seizures
5.PHENOBARBITONE
- Action
- potentiate GABA receptor activation
- CYP450 inducer
- half life 72 - 144 h
- ADE
- sedation with therapeutic levels
- changes in cognition, mood & behaviour
- megaloblastic changes
- osteomalacia
- hypersensitive reaction
- addiction
- depress brain stem functions
- coma, respiratory failure, cardiac arrest
6.CLONAZAPAM
- Action
- enhance GABA receptor activation
- T type Ca channel inhibition
- ADE
- sedation
- tolerance with prolong use
7.VIGABATRIN
- Action
- Irreversible inhibition of GABA transaminases
- ADE
- tunnel vision - 6 month visual field monitoring
8.GABAPENTIN
- Action
- inhibit Glutamate release by blocking high voltage Ca channels
- No effect on metabolizing enzymes
- eliminated unchanged in urine
- half life is 6h so given tds
- ADE
- sedation
- fatigue
- weightgain
- Uses
- adjunctive therapy for partial seizures
9.TOPIRAMATE
- Action
- Na ,Ca channel block
- GABA potentiation
- Glutamate receptor block
- Carbonic anhydrase inhibitor
- ADE
- sedation
- fatigue
- renal calculi
- weight loss
- increased intra occular pressure
10.LEVATIRACETAM
- Action
- inhibit Glutamate release
- renal elimination- unchanged
- Uses
- migraine prevention
- partial seizures
11.ETHOSUXIMIDE
Carbamezapine is relatively safe in pregnancy with vit K & folic acid supplementation.
- valproate - neural tube defects
- phenytoin - cleft palate
- phenobarbitone - cardiac malformations
- valproate - neural tube defects
- phenytoin - cleft palate
- phenobarbitone - cardiac malformations
Drugs according to the mechanism of action- Ion channel block
- Na - phenytoin, carbemezapine, lamotrigine, Na valproate, topiramate
- Ca - lamotrigiine, Na valproate, topiramate, ethosuximide
- Reduce Glutamate activity - lamotrigine, gabapentine, topiramate, livetiracetam
- Increase GABA activity
Drugs according to the mechanism of action
- Ion channel block
- Na - phenytoin, carbemezapine, lamotrigine, Na valproate, topiramate
- Ca - lamotrigiine, Na valproate, topiramate, ethosuximide
- Reduce Glutamate activity - lamotrigine, gabapentine, topiramate, livetiracetam
- Increase GABA activity
- increase post synaptic action of GABA -phenobarbitone, clonezapam, Na valproate, topiramate,
- decrease GABA transaminases - Vigabatrin, Na valproate
- decrease GABA re uptake in to glial cells - Tigabine
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